|Systematic (IUPAC) name|
|Mol. mass||395.536 g/mol|
WAY-100,135 is a serotonergic drug of the phenylpiperazine family which is used in scientific research. It acts as potent 5-HT1A receptor antagonist, and was originally believed to be highly selective, but further studies have demonstrated that it also acts as a partial agonist of the 5-HT1D receptor (pKi = 7.58; virtually the same affinity for 5-HT1A), and to a much lesser extent, of the 5-HT1B receptor (pKi = 5.82). These findings may have prompted the development of the related compound WAY-100,635, another purportedly selective and even more potent 5-HT1A antagonist, which was synthesized shortly thereafter. However, WAY-100,635 turned out to be non-selective as well, having been shown to act additionally as a potent D4 receptor agonist later on.
- Fletcher A, Bill DJ, Bill SJ, et al. (June 1993). "WAY100135: a novel, selective antagonist at presynaptic and postsynaptic 5-HT1A receptors". European Journal of Pharmacology 237 (2-3): 283–91.
- Cliffe IA, Brightwell CI, Fletcher A, et al. (May 1993). "(S)-N-tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors". Journal of Medicinal Chemistry 36 (10): 1509–10.
- Davidson C, Ho M, Price GW, Jones BJ, Stamford JA (June 1997). "(+)-WAY 100135, a partial agonist, at native and recombinant 5-HT1B/1D receptors".
- Fornal CA, Metzler CW, Gallegos RA, Veasey SC, McCreary AC, Jacobs BL (August 1996). "WAY-100635, a potent and selective 5-hydroxytryptamine1A antagonist, increases serotonergic neuronal activity in behaving cats: comparison with (S)-WAY-100135". The Journal of Pharmacology and Experimental Therapeutics 278 (2): 752–62.
- Chemel BR, Roth BL, Armbruster B, Watts VJ, Nichols DE (October 2006). "WAY-100635 is a potent dopamine D4 receptor agonist". Psychopharmacology 188 (2): 244–51.